IP Library › Granted Patent US 45,313
Granted Patent E1
US 45,313 · App. 13/944,735 · Granted Dec 30, 2014

Exendin variant peptides

Inventors: Bjarne Due Larsen (Roskilde, DK); Jens Damsgaard Mikkelsen (Kgs. Lyngby, DK); Søren Neve (Kgs. Lyngby, DK)
Assignee: Zealand Pharma A/S
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Quick Facts
Patent No.
US 45,313
App. No.
13/944,735
Granted
Dec 30, 2014
Kind
E1
Abstract

The present invention relates to novel peptide conjugates which have increased stability and are useful in the treatment of excess levels of blood glucose.

Claims (13)

1. A peptide consisting of any one of the following sequences:

a) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-(Lys) 6 -NH 2 (des-Pro 36 -exendin-4(1-39)-Lys 6 -NH 2 ) (SEQ ID NO:93),

b) H-Lys 6 -His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-(Lys) 6 -NH 2 (H-Lys 6 -des Pro 36 exendin-4(1-39)-Lys 6 -NH 2 ) (SEQ ID NO: 149),

c) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-NH 2 (H-des Pro 36 ,Pro 37 ,Pro 38 exendin-4 (1-39)-NH 2 ) (SEQ ID NO: 132),

d) H-Lys-Lys-Lys-Lys-Lys-Lys-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-NH 2 (H-(Lys) 6 -des Pro 36 ,Pro 37 ,Pro 38 exendin-4(1-39)-NH 2 ), (SEQ ID NO: 134),

e) H-Asn-Glu-Glu-Glu-Glu-Glu-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-NH 2 (H-Asn-(Glu) 5 -des Pro 36 ,Pro 37 , Pro 38 exendin-4(1-39)-NH 2 ) (SEQ ID NO: 137),

f) H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Lys) 6 -NH 2 (des Pro 36 , Pro 37 ,Pro 38 exendin-4 (1-39)-(Lys) 6 -NH 2 ) (SEQ ID NO: 133),

g) H-(Lys) 6 -His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Lys) 6 -NH 2 (H-(Lys) 6 -des Pro 36 ,Pro 37 , Pro 38 exendin-4(1-39)-(Lys) 6 -NH 2 ) (SEQ ID NO: 135),

h) H-Asp-Glu-Glu-Glu-Glu-Glu-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Ser-(Lys) 6 -NH 2 (H-Asn-(Glu) 5 -des Pro 36 ,Pro 37 ,Pro 38 exendin-4(1-39)-(Lys) 6 -NH 2 ) (SEQ ID NO: 136);

or a pharmaceutically acceptable salt thereof.

2. A composition comprising the peptide of claim 1 and a physiologically acceptable carrier.

3. A peptide consisting of the sequence H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-(Lys) 6 -NH 2 (des-Pro 36 -exendin-4(1-39)-Lys 6 -NH 2 ) (SEQ ID NO:93), or a pharmaceutically acceptable salt thereof.

4. A composition comprising the peptide of claim 3 and a physiologically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 20, 2015
From: LARSEN, BJARNE DUE; MIKKELSEN, JENS DAMSGAARD; NEVE, SØREN
To: ZEALAND PHARMA A/S
Reel/Frame 036382/0163 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 20, 2015
From: ZEALAND PHARMA A/S
To: ZP HOLDING SPV K/S
Reel/Frame 036382/0399 →
Continuity (2)
Reissue 09614847 · Jul 12, 2000
Provisional Application 60143591 · Jul 12, 1999